CN1872030B - Drop pills of anticancer drugs, and preparation method - Google Patents
Drop pills of anticancer drugs, and preparation method Download PDFInfo
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- CN1872030B CN1872030B CN2005100136125A CN200510013612A CN1872030B CN 1872030 B CN1872030 B CN 1872030B CN 2005100136125 A CN2005100136125 A CN 2005100136125A CN 200510013612 A CN200510013612 A CN 200510013612A CN 1872030 B CN1872030 B CN 1872030B
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- 238000000034 method Methods 0.000 claims abstract description 17
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- 239000002671 adjuvant Substances 0.000 claims description 60
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Abstract
A dripping pill of anticancer medicine for treating cancer features high natural level and safety and low toxic by-effect. Its preparing process is also disclosed.
Description
Technical field
The present invention relates to field of medicaments, particularly, relating to Chinese medicine is that raw material is made a kind of medicine for the treatment of cancer.
Background technology
Cancer is the very high disease of present fatality rate, therefore how to prolong cancer patient's life, how to improve cancer patient's quality of life, is the key issue for the treatment of cancer at present.
The effective ingredient of the cancer therapy drug that camptothecine, paclitaxel, harringtonine, homoharringtonine are the most natural is widely used in the treatment for cancer.Application number: 03130885.6, the applying date: 2003.5.21, applicant: Liu Zhi, denomination of invention: a kind of have the oral administration dripping pill of anti-cancer alkaloid and the patent documentation of preparation method provides a kind of drop pill oneself for the treatment of cancer and preparation method thereof, and this drop pill drug use Polyethylene Glycol and other adjuvants are made drop pill with anti-cancer alkaloid; Though this drop pill overcomes the defective of present injectable powder, there is the not high defective of natural degree of the adjuvant that uses in this drop pill.
Expansion and human back to nature requirement along with the market global range, use the low medicine of toxic and side effects, especially pure natural medical more and more becomes people's first-selection, dropping pill formulation be a kind of have efficient, quick-acting new medicine preparations, it has overcome the shortcoming and deficiency of Chinese medicine preparation in the past, but present dropping pill formulation generally faces following problem: 1, drop pill adjuvant pure natural degree is not high: at present, drop pill substrate adjuvant mostly is synthetic, natural degree is lower, the searching of new alternative substrate adjuvant, the searching of the alternative substrate adjuvant that particularly natural degree is high and preparation technology thereof determine, it is again very difficult thing, because the required preparation condition of at present common possible natural substrates adjuvant succedaneum is very harsh, it all is to influence the key that drop pill prepares molding that adjuvant temperature and drop pill thereof drip the system condition.The too high then viscosity of adjuvant melt temperature is low, and poor plasticity is though the adjuvant melt temperature is crossed lowplastcity by force, but drop pill has shortcomings such as easily sticking ball, distortion, therefore, seek pure natural degree height, and the adjuvant that is suitable for substituting existing drop pill substrate is a very job of hardships.2, the drop pill outlet encounters problems: along with expanding economy, more and more internationalize in market, China is also just making great efforts to adapt to this trend, present Chinese medicine dripping pills preparation as health food, successful export to many countries, but also face many problems at present, because different countries is different to the approval of the selected adjuvant of Chinese medicine dropping pill formulation, especially industrial flourishing Europe, more strict to food adjuvant and medical auxiliary materials, and as the selected chemosynthesis adjuvant (as Polyethylene Glycol) of the dropping pill formulation of health food outlet not in the catalogue of some national food additive, it is very unfavorable that this moves towards the international market to the Chinese medicine dropping pill formulation, becomes the stumbling-block that Chinese medicine enters the international market, therefore, seek the new of one or more, can be particularly important, also very urgent for the substrate adjuvant that the international market is accepted.3, the shortcoming of mouthfeel and onset speed: the mouthfeel of Chinese medicine and preparation thereof is relatively poor to be the big characteristics of one, people when taking some drugs to the frightened of disagreeable taste that medicine had even be better than fear far away to disease, What is more, some patients are because can not overcome the poor taste of Chinese medicine or its preparation or abnormal smells from the patient and abandon the treatment of Chinese medicine, though can improve mouthfeel as medicine being made capsule or sugar coated tablet, reducing stimulates, but disintegration rate prolongs, be unfavorable for the rapid onset of medicine, to some disease, particularly need the disease of the rapid onset of medicine inapplicable.4, the preparation process difficulty of drop pill suitability for industrialized production: in the replacement process of dropping pill formulation adjuvant, determining of the preparation process of its suitability for industrialized production is very difficult something, as the ratio of the melt temperature of substrate adjuvant, the proportioning of dripping system temperature, adjuvant and medicine, dropper bore, condensing agent etc. all are the factors that influence drop pill, therefore, the replacement of substrate and to be suitable for suitability for industrialized production be a job consuming time, as to expend substantial contribution.
In order to change drop pill substrate adjuvant for a long time based on the situation of chemosynthesis adjuvant, it is low to solve the pure natural degree that present drop pill substrate faced, and can not satisfy more and more that people require back to nature, take low toxicity, the problem of the pure natural medical that has no side effect; Also can solve some problems that Chinese medicine preparation, particularly dropping pill formulation are run in exit procedure, strengthen the competitiveness of international market; The present invention has invented the pure Chinese medicine dripping pills preparation that a kind of toxic and side effects is low, evident in efficacy, moderate, adapt to industrialized great production by a large amount of tests and the research of preparation process.
Summary of the invention
The medicine that the purpose of this invention is to provide a kind of treatment cancer with new type natural substrate adjuvant preparation.
Another object of the present invention provides a kind of preparation method for the treatment of cancer drug.
The selected substrate adjuvant of the present invention is resulting by a large amount of tests, it is little to have molecular weight, soluble in water, and molten diffusing speed is faster, pure natural degree height, toxic and side effects is low, and can reduce the medicine irritation abnormal smells from the patient, has the oral cavity of improvement acid-base value during the buccal of oral cavity, improve the characteristics of oral cavity smell, the used substrate adjuvant of the present invention is the agent of food sedan-chair flavor, takes that mouthfeel is good, the acceptant characteristics of patient, is the direction of following substrate adjuvant development.
The consumption of drug component of the present invention and the selection of adjuvant thereof also grope to sum up to draw through the inventor in a large number, and this medicine comprises anti-cancer alkaloid active component, appropriate amount of auxiliary materials; Wherein adjuvant comprises filler and plasticity substrate, and filler adjuvant wherein is selected from the natural adjuvant of following one or more plant origins: sorbitol, xylitol, lactose, maltose, and they contain the water of crystallization chemical compound; Plasticity substrate wherein is selected from following one or more the natural adjuvant of plant origin: pregelatinized Starch, carboxymethyl starch, methylcellulose, sodium carboxymethyl cellulose, hydroxypropyl emthylcellulose, arabic gum, alginic acid, dextrin, cyclodextrin, agar, lactose.
Anti-cancer alkaloid active component wherein is selected from one or several in camptothecine, paclitaxel, harringtonine, the homoharringtonine.
The adjuvant of preferred drug component of the present invention is following one or more the natural adjuvant of plant origin for the filler adjuvant is selected from: xylitol, lactose; Plasticity substrate wherein is selected from following one or more the natural adjuvant of plant origin: starch, arabic gum;
Best substrate adjuvant of the present invention is xylitol and starch, and xylitol is 1: 0.2～1: 0.3 with the ratio of the weight of starch; Or be lactose and starch, lactose is 1: 0.2～1: 0.3 with the ratio of the weight of starch; Or be xylitol and arabic gum, the ratio of the weight of xylitol and arabic gum is 1: 0.2～1: 0.4.
Adjuvant is 1: 0.1～1: 1 with the ratio of the weight of anti-cancer alkaloid active component in the pharmaceutical composition of the present invention;
Adjuvant is 1: 0.1～1: 0.6 with the ratio of the weight of anti-cancer alkaloid active component in the preferred pharmaceutical composition of the present invention;
Adjuvant is 1: 0.2～1: 0.4 with the ratio of the weight of anti-cancer alkaloid active component in the best pharmaceutical composition of the present invention.
Medicine mesostroma adjuvant of the present invention and amount of drug are than being the scope that allows on the galenic pharmacy, and medicine described here can be that crude drug also can be the effective ingredient extract.
Medicine of the present invention can adopt the preparation of Chinese medicine preparation conventional method; make common any preparation at present; but, preferably adopt following method to be prepared into dropping pill formulation, but this can not limit protection scope of the present invention in order to make each crude drug of this medicine bring into play drug effect better.
The preparation method of medicine of the present invention is as follows:
(a) get anti-cancer alkaloid, adjuvant is standby;
(b) in appropriate amount of auxiliary materials, add the anti-cancer alkaloid active component, fully mix, mixture is at 45～115 ℃ of heating and meltings, stir, mixing time is 1～120 minute, insulation, at 45～95 ℃ of temperature following system, dropper bore is 1.0～4.0 millimeters, splash in-20～25 ℃ liquid paraffin, methyl-silicone oil or the vegetable oil, with the drop pill drop to the greatest extent and wipe liquid coolant, promptly.
Further preferred manufacturing procedure is:
The mixture heated melt temperature is 60～85 ℃ in the step (b), and mixing time is 10～30 minutes, and dripping a system temperature and be 60～85 ℃, dropper bore is 1.1～3.5 millimeters, and condensing agent is 0～18 ℃ liquid paraffin or a methyl-silicone oil.
Best preparation method is:
The mixture heated melt temperature is 64 ℃ in the step (b), and dripping a system temperature and be 64 ℃, dropper bore is 1.2～2.5 millimeters, and condensing agent is 0 ℃ a methyl-silicone oil.
More than form when producing and to increase or to reduce according to corresponding ratio, as large-scale production can be unit with kilogram or with the ton, small-scale production can be unit with the gram also, and weight can increase or reduce, but the crude drug material weight proportion constant rate between each composition.
Medicine of the present invention can be determined usage and dosage according to patient's situation in use, but every day 1-3 time, and every day, each crude drug consumption was as the criterion with the state-promulgated pharmacopoeia dosage, was no more than the pharmacopeia ormal weight.
The drop pill that the present invention is prepared, conventional drop pill advantage is simple as preparing except having, steady quality, can make liquid medicine solidification, convenient drug administration, efficient, quick-acting, its biggest advantage is:
1, the selected adjuvant pure natural of the present invention degree height: the substrate adjuvant that employed substrate adjuvant derives from natural plants or originates based on natural plants among the present invention, for example: selected substrate adjuvant is xylitol and starch or lactose and starch or xylitol and arabic gum, this substrate adjuvant has pure natural degree height, toxic and side effects is low, mouthfeel is good, dissolve scattered time limit is short, rapid-action, it is a kind of new medium adjuvant, can be used for substituting present chemosynthesis substrate adjuvant, the drop pill made from this kind adjuvant, it is low to solve the pure natural degree that present drop pill substrate faced, and more and more can not satisfy people and require back to nature, take low toxicity, the problem of the pure natural medical that has no side effect.
2, some problems in the outlet of solution Chinese medicine: medicine of the present invention also can solve Chinese medicine preparation, some problems of in exit procedure, being run into of dropping pill formulation particularly, solve because different countries, especially the European countries of industry prosperity are to the difference identification of the selected adjuvant of Chinese medicine dropping pill formulation, overcome as the selected adjuvant Polyethylene Glycol of the dropping pill formulation of the health food outlet defective in some national food additive catalogue not, improve the Chinese medicine dripping pills preparation and move towards the international market, strengthen the competitiveness of international market.
3, solve the relatively poor problem of drop pill taste and further improve drug effect speed (dissolve scattered time limit): the medicinal dropping ball made from this kind substrate adjuvant of the present invention, can improve Chinese medicine preparation, the particularly present not good shortcoming of dropping pill formulation taste, improve mouthfeel, more easy for patients to accept, and the drop pill that adopts the selected adjuvant of medicine of the present invention to make has shorter dissolve scattered time limit, making drug effect faster, is the medicine that cancer is treated in a kind of onset faster.
4, higher safety and solve some problems in the drop pill storage process: the selected substrate of the present invention is not only additive, nutrient commonly used in the food industry, and can do medicinal, but do not see that it uses as the drug matrices adjuvant, therefore, with regard to substrate, be perfectly safe, have no side effect, a large amount of evidences, the drop pill that this adjuvant is made can reduce effective ingredient separating out in storage process, the sticking ball of drop pill, easy shortcomings such as moisture absorption deliquescing, but the big production of suitability for industrialized.
The present invention is under instruction of Chinese Medicine theory, tests resulting preparation through a large amount of preparation technologies.The present invention is used for the treatment of cancer clinically, has overcome that western medicine cancer toxic and side effects is big, expense is high, and the Chinese medicine curative effect is low, flavour of a drug are many, the shortcoming of incompatibility large-scale production, is the medicine of the definite treatment cancer of a kind of economy, material benefit, curative effect.
To those skilled in the art, technology contents disclosed according to the present invention, those skilled in the art will very clear other embodiment of the present invention, and the embodiment of the invention is only as example.Under the situation of not violating purport of the present invention and scope, can carry out various changes and improvements to the present invention.For example, use different crude drug or extract or active constituents of medicine or effective ingredient and adjuvant provided by the present invention to make various different preparations, particularly drop pill, but as long as use adjuvant of the present invention, all within protection domain of the present invention.
In order to understand the present invention better, the drop pills of anticancer drugs made from the new substrate of the present invention (according to embodiment 1 preparation, hereinafter to be referred as the new anti-cancer drug composition dropping pills) below; Test explanation advantages of the present invention such as the dissolve scattered time limit of the drop pill of making for the substrate adjuvant with the Polyethylene Glycol (according to application number be: 03130885.6 specific embodiment 1 prepares, hereinafter to be referred as old drop pills of anticancer drugs), drop pill soft durometer, the sticking ball of drop pill.
Test example 1: dissolve scattered time limit, weight differential contrast experiment's example
In vitro tests
New anti-cancer drug composition dropping pills and old drop pills of anticancer drugs compare, and by measuring dissolve scattered time limit, investigate its good releasing effect; By measuring indexs such as the ball method of double differences is different, whether ripe, whether be fit to suitability for industrialized production if investigating its preparation technology.
1. test medication: new anti-cancer drug composition dropping pills, old drop pills of anticancer drugs.
2. method and result:
Dissolve scattered time limit: by " method is measured under this item of Chinese pharmacopoeia; The ball method of double differences is different: by " method is measured under this item of Chinese pharmacopoeia.Result of the test sees Table 1.
Three batches in table 1 with new anti-cancer drug composition dropping pills and old drop pills of anticancer drugs dissolve scattered time limit, weight differential relatively
Above-mentioned experimental data shows that the older drop pills of anticancer drugs of the dissolve scattered time limit of new anti-cancer drug composition dropping pills is few, different being controlled in the pharmacopeia prescribed limit of the ball method of double differences new, old drop pills of anticancer drugs.The result of the test explanation, the new anti-cancer drug composition dropping pills that the new medium adjuvant is made is more conducive to medicine and plays a role in the shortest time, different all being controlled in the pharmacopeia prescribed limit of the ball method of double differences new, old drop pills of anticancer drugs, but suitability for industrialized production.
Test example 2: the comparative observation of new anti-cancer drug composition dropping pills and old drop pills of anticancer drugs soft durometer, the sticking ball of drop pill
Compare by new anti-cancer drug composition dropping pills and old drop pills of anticancer drugs, measure indexs such as above-mentioned, investigate its effect.
1. test medication: new anti-cancer drug composition dropping pills; Old drop pills of anticancer drugs.
2. method and result:
Get each three batches of new anti-cancer drug composition dropping pills and old drop pills of anticancer drugs, be loaded in the porcelain vase respectively, and use the bottle stopper good seal.Putting it into the bottom has in the exsiccator of saturated Nacl (humidity 75%) solution, exsiccator is put into 40 ℃ of drying baker of constant temperature again, and timing sampling is observed situations such as drop pill soft durometer, the sticking ball of drop pill, the results are shown in Table 2.1, table 2.2.
Three batches of old drop pills of anticancer drugs reserved sample observings of table 2.1 relatively
Table 2.2: three batches of new anti-cancer drug composition dropping pills and old drop pills of anticancer drugs character observation are relatively
Table 2.1,2.2 test data show that new anti-cancer drug composition dropping pills soft durometer changes similar to old drop pills of anticancer drugs, strong slightly; The new anti-cancer drug composition dropping pills glues the ball variation, firmness change is similar to old drop pills of anticancer drugs.The result of the test explanation, the sticking ball of new, old drop pills of anticancer drugs changes, firmness change is similar, and the alternative present chemosynthesis adjuvant of this natural substrates adjuvant is described, but suitability for industrialized production.
The specific embodiment
Embodiment 1
(a) get camptothecine 10g, xylitol 83.3g, starch 16.7g is standby;
(b) get xylitol and starch mix homogeneously, adding above-mentioned paclitaxel fully mixes, mixture stirs at 64 ℃ of heating and meltings, and mixing time is 10～30 minutes, insulation, at 64 ℃ of temperature following system, dropper bore is 1.2～2.5 millimeters, splashes in 0 ℃ the methyl-silicone oil, makes 5000 drop pill, with the drop pill drop to the greatest extent and wipe liquid coolant, promptly.
Embodiment 2
(a) get paclitaxel 20g, lactose 76.9g, starch 23.1g is standby;
(b) get lactose and starch mix homogeneously, adding above-mentioned paclitaxel fully mixes, mixture stirs at 64 ℃ of heating and meltings, and mixing time is 10～30 minutes, insulation, at 64 ℃ of temperature following system, dropper bore is 1.2～2.5 millimeters, splashes in 0 ℃ the methyl-silicone oil, makes 5000 drop pill, with the drop pill drop to the greatest extent and wipe liquid coolant, promptly.
Embodiment 3
(a) get harringtonine 40g, xylitol 71.4g, arabic gum 28.6g is standby;
(b) get xylitol and arabic gum mix homogeneously, adding above-mentioned harringtonine fully mixes, mixture stirs at 64 ℃ of heating and meltings, and mixing time is 10～30 minutes, insulation, at 64 ℃ of temperature following system, dropper bore is 1.2～2.5 millimeters, splashes in 0 ℃ the methyl-silicone oil, makes 5000 drop pill, with the drop pill drop to the greatest extent and wipe liquid coolant, promptly.
Embodiment 4
(a) get homoharringtonine 60g, xylitol 80g, starch 20g is standby;
(b) get xylitol and starch mix homogeneously, adding above-mentioned homoharringtonine fully mixes, mixture stirs at 45～70 ℃ of heating and meltings, and mixing time is 10～30 minutes, insulation, at 60～70 ℃ of temperature following system, dropper bore is 1.21～2.5 millimeters, splashes in-10～10 ℃ the methyl-silicone oil, makes 6000 drop pill, with the drop pill drop to the greatest extent and wipe liquid coolant, promptly.
Embodiment 5
(a) get harringtonine 12.5g, homoharringtonine 12.5g, xylitol 62.5g, starch 37.5g are standby;
(b) get xylitol and starch mix homogeneously, add above-mentioned harringtonine and homoharringtonine, mixture stirs at 45～115 ℃ of heating and meltings, and mixing time is 1～30 minute, insulation, at 45～95 ℃ of temperature following system, dropper bore is 1.0～4.0 millimeters, splashes in-20～25 ℃ the vegetable oil, makes 3000 drop pill, with the drop pill drop to the greatest extent and wipe liquid coolant, promptly.
Embodiment 6
(a) get camptothecine 1g, paclitaxel 2g, harringtonine 3g, homoharringtonine 5g, maltose 100g is standby;
(b) get maltose and add above-mentioned camptothecine, paclitaxel, harringtonine, homoharringtonine, mixture is at 55～75 ℃ of heating and meltings, stir, mixing time is 5～12 minutes, and insulation is 1.20～3.0 millimeters at 55～75 ℃ of temperature following system, dropper bore, splash in 0～15 ℃ the liquid paraffin, make 5000 drop pill, with the drop pill drop to the greatest extent and wipe liquid coolant, promptly
Embodiment 7
(a) get camptothecine 10g, paclitaxel 10g, xylitol 80g, cyclodextrin 20g are standby;
(b) get xylitol and cyclodextrin mixing mixing, add above-mentioned camptothecine, paclitaxel, mixture stirs at 45～115 ℃ of heating and meltings, mixing time is 5～20 minutes, and insulation is dripped system 58～70 ℃ of insulations, splash in 12 ℃ of liquid paraffin, make 4000 drop pill of drop pill, promptly.
Embodiment 8
(a) get camptothecine 8g, homoharringtonine 5g, xylitol 99g, pregelatinized Starch 7g are standby;
(b) get xylitol and pregelatinized Starch mix homogeneously, add above-mentioned camptothecine, homoharringtonine, mixture stirs at 60～755 ℃ of heating and meltings, and mixing time is 10～60 minutes, insulation, at 55～65 ℃ of temperature following system, dropper bore is 1.0～3.5 millimeters, splashes in-20～25 ℃ the vegetable oil, makes 3000 drop pill, with the drop pill drop to the greatest extent and wipe liquid coolant, promptly.
Embodiment 9
(a) get paclitaxel 11.5g, harringtonine 12.5g, lactose 66g, starch 34g are standby;
(b) get mixing of lactose and starch, add above-mentioned paclitaxel, harringtonine, mixture stirs at 60～85 ℃ of heating and meltings, and mixing time is 10～30 minutes, insulation, at 60～85 ℃ of temperature following system, dropper bore is 1.1～3.5 millimeters, splashes in 0～18 ℃ the methyl-silicone oil, makes 3000 drop pill, with the drop pill drop to the greatest extent and wipe liquid coolant, promptly.
Embodiment 10
(a) get paclitaxel 5g, harringtonine 6g, homoharringtonine 7g, xylitol 62.5g, arabic gum 37.5g is standby;
(b) get the mixing mixing of xylitol and arabic gum, add above-mentioned paclitaxel, harringtonine, homoharringtonine, mixture stirs at 60～85 ℃ of heating and meltings, and mixing time is 10～30 minutes, insulation, at 60～85 ℃ of temperature following system, dropper bore is 1.1～3.5 millimeters, splashes in 0～18 ℃ the liquid paraffin, makes 3000 drop pill, with the drop pill drop to the greatest extent and wipe liquid coolant, promptly.
Embodiment 11
(a) get camptothecine 45g, xylitol 80g, alginic acid 20g is standby;
(b) get xylitol and alginic acid mixing mixing, camptothecine in the adding, mixture stirs at 60～85 ℃ of heating and meltings, and mixing time is 10～30 minutes, insulation, at 60～85 ℃ of temperature following system, dropper bore is 1.21～3.5 millimeters, splashes in 0～15 ℃ the methyl-silicone oil, makes 10000 drop pill, with the drop pill drop to the greatest extent and wipe liquid coolant, promptly.
Embodiment 12
(a) get paclitaxel 50g, xylitol 166g, sodium carboxymethyl cellulose 34g is standby;
(b) get xylitol and sodium carboxymethyl cellulose mix homogeneously, add above-mentioned paclitaxel, mixture stirs at 60～85 ℃ of heating and meltings, and mixing time is 10～20 minutes, insulation, at 60～75 ℃ of temperature following system, dropper bore is 1.5～3.5 millimeters, splashes in 10～18 ℃ the liquid paraffin, makes 10000 drop pill, with the drop pill drop to the greatest extent and wipe liquid coolant, promptly.
Embodiment 13
(a) get harringtonine 5.5g, lactose 40g, agar 10g is standby;
(b) get lactose and agar mix homogeneously, add above-mentioned harringtonine, mixture stirs at 60～70 ℃ of heating and meltings, and mixing time is 10～30 minutes, insulation, at 62～67 ℃ of temperature following system, dropper bore is 1.2～2.5 millimeters, splashes in 4 ℃ the methyl-silicone oil, makes 2000 drop pill, with the drop pill drop to the greatest extent and wipe liquid coolant, promptly.
Embodiment 14
(a) get homoharringtonine 55g, xylitol 85g, arabic gum 15g is standby;
(b) get xylitol and arabic gum mix homogeneously, add above-mentioned homoharringtonine, mixture stirs at 55～85 ℃ of heating and meltings, and mixing time is 5～30 minutes, insulation, at 58～68 ℃ of temperature following system, dropper bore is 1.21～2.5 millimeters, splashes in 0 ℃ the methyl-silicone oil, makes 10000 drop pill, with the drop pill drop to the greatest extent and wipe liquid coolant, promptly.
Embodiment 15
(a) get paclitaxel 50g, lactose 70g, hydroxypropyl emthylcellulose 20g is standby;
(b) getting lactose and hydroxypropyl emthylcellulose mixes, add above-mentioned paclitaxel, fully mix, mixture is at 64 ℃ of heating and meltings, stir, mixing time is 10～30 minutes, and insulation is 1.2～2.5 millimeters at 64 ℃ of temperature following system, dropper bore, splash in 0 ℃ the methyl-silicone oil, make 10000 drop pill, with the drop pill drop to the greatest extent and wipe liquid coolant, promptly.
Embodiment 16
(a) get harringtonine 4g, xylitol 60g, methylcellulose 40g is standby;
(b) get xylitol and methylcellulose mixing, adding above-mentioned harringtonine fully mixes, mixture stirs at 60～70 ℃ of heating and meltings, and mixing time is 10～30 minutes, insulation, at 62～66 ℃ of temperature following system, dropper bore is 1.2～2.5 millimeters, splashes in 0 ℃ the methyl-silicone oil, makes 1000 drop pill, with the drop pill drop to the greatest extent and wipe liquid coolant, promptly.
Claims (5)
1. a drop pills of anticancer drugs is characterized in that this medicine consists of: camptothecine 10g, xylitol 83.3g, starch 16.7g.
2. drop pill as claimed in claim 1 is characterized in that adopting following method preparation:
(a) get camptothecine 10.0g, xylitol 83.3g, starch 16.7g is standby;
(b) get xylitol and starch mix homogeneously, adding above-mentioned camptothecine fully mixes, mixture stirs at 64 ℃ of heating and meltings, and mixing time is 10～30 minutes, insulation, at 64 ℃ of temperature following system, dropper bore is 1.2～2.5 millimeters, splashes in 0 ℃ the methyl-silicone oil, makes 5000 drop pill, with the drop pill drop to the greatest extent and wipe liquid coolant, promptly.
3. the preparation method of the described drop pill of claim 1 is characterized in that this method comprises the steps:
(a) get camptothecine, adjuvant is standby;
(b) in appropriate amount of auxiliary materials, add camptothecine, fully mix, mixture is at 45～115 ℃ of heating and meltings, stir, mixing time is 1～120 minute, insulation, at 45～95 ℃ of temperature following system, dropper bore is 1.0～4.0 millimeters, splash in-20～25 ℃ liquid paraffin, methyl-silicone oil or the vegetable oil, with the drop pill drop to the greatest extent and wipe liquid coolant, promptly.
4. the preparation method of drop pill as claimed in claim 3, it is characterized in that the mixture heated melt temperature is 60～85 ℃, mixing time is 10～30 minutes, and dripping a system temperature and be 60～85 ℃, dropper bore is 1.1～3.5 millimeters, and condensing agent is 0～18 ℃ liquid paraffin or a methyl-silicone oil.
5. the preparation method of drop pill as claimed in claim 4 is characterized in that the mixture heated melt temperature is 64 ℃, and dripping a system temperature and be 64 ℃, dropper bore is 1.2～2.5 millimeters, and condensing agent is 0 ℃ a methyl-silicone oil.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2005100136125A CN1872030B (en) | 2005-06-01 | 2005-06-01 | Drop pills of anticancer drugs, and preparation method |
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| CN2005100136125A CN1872030B (en) | 2005-06-01 | 2005-06-01 | Drop pills of anticancer drugs, and preparation method |
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Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1462617A (en) * | 2003-05-21 | 2003-12-24 | 刘智 | Alkaloid oral applied drop pills possessing anticarcinogenesis and its preparation method |
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Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1462617A (en) * | 2003-05-21 | 2003-12-24 | 刘智 | Alkaloid oral applied drop pills possessing anticarcinogenesis and its preparation method |
Non-Patent Citations (1)
| Title |
|---|
| 王薇.新基质复方丹参滴丸的研究.第二军医大学学位论文.2004,第7、24、26、62页. * |
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